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    • 4. 发明专利
    • Method for forming amorphous atorvastatin calcium
    • 形成无定形ATORVASTATIN钙的方法
    • JP2008255117A
    • 2008-10-23
    • JP2008105757
    • 2008-04-15
    • Pfizer Prod Incファイザー・プロダクツ・インク
    • ROSE PETER ROBERTLEONARD JASON ALBERT
    • C07D207/34
    • C07D207/34
    • PROBLEM TO BE SOLVED: To provide an improved method for producing an amorphous atorvastatin calcium in order to solve the problems that the existing production method of the amorphous atorvastatin includes non-best solvent from the view point of toxicity and environment, and the existing method is non-best from the view point of production ability and is improper in large scale synthesis.
      SOLUTION: An amorphous atorvastatin hemi calcium salt trihydrate is formed by a method comprising following steps: (a) dissolving the atorvastatin in a solvent to form a solution, and (b) adding the solution in a mixture comprising a non-solvent and a hydroxy solvent to precipitate the atorvastatin from the solution and to obtain the amorphous atorvastatin.
      COPYRIGHT: (C)2009,JPO&INPIT
    • 要解决的问题:为了解决从毒性和环境的观点出发,无定形阿托伐他汀的现有生产方法包括非最佳溶剂的问题,提供了一种制备无定形阿托伐他汀钙的改进方法, 从生产能力的观点来看,现有的方法是非常好的,在大规模合成中是不合适的。 解决方案:通过包括以下步骤的方法形成无定形阿托伐他汀半钙盐三水合物:(a)将阿托伐他汀溶解在溶剂中以形成溶液,和(b)将溶液加入到包含非溶剂的混合物 和羟基溶剂,从溶液中沉淀阿托伐他汀,得到无定形的阿托伐他汀。 版权所有(C)2009,JPO&INPIT
    • 9. 发明专利
    • Pharmaceutical composition comprising drug and concentration-enhancing polymer
    • 包含药物和浓度增加聚合物的药物组合物
    • JP2008044967A
    • 2008-02-28
    • JP2007278603
    • 2007-10-26
    • Pfizer Prod Incファイザー・プロダクツ・インク
    • CURATOLO WILLIAM JOHNDWAYNE THOMAS FREESEN
    • A61K9/00A61K47/38A61K9/06A61K9/10A61K9/107A61K9/14A61K9/20A61K31/404A61K31/4045A61K31/47A61K31/4706A61K31/496A61K31/58A61K31/724A61K47/32A61K47/34A61K47/36A61K47/40A61K47/42A61K47/48A61P5/32A61P15/00A61P25/18A61P43/00
    • B82Y5/00A61K9/145A61K9/146A61K31/724A61K47/6951
    • PROBLEM TO BE SOLVED: To provide a pharmaceutical composition comprising a drug and a concentration-enhancing polymer. SOLUTION: The composition comprises (a) a drug in a solubility-improved form which provides, when administered to a use environment, at least one of a dissolved drug concentration in the use environment that exceeds an equilibrium concentration of a lowest solubility form of the drug in the use environment and a dissolution rate that exceeds a dissolution rate of the lowest solubility form of the drug in the use environment, and (b) a concentration-enhancing polymer which concentration-enhancing polymer is present in a sufficient amount so that the composition provides, after introduction to the use environment, a maximum concentration of the drug in the use environment that is at least 1.25-fold a maximum concentration of the drug provided by a control composition which control composition is an equivalent quantity of the drug in the solubility-improved form alone, wherein the solubility-improved drug form is selected from the group consisting of drug in nanoparticulate form, absorbed drug, drug in a nanosuspension, a supercooled melt of drug, cyclodextrin/drug form, gelatin form, softgel form, self-emulsifying form, and three-phase drug form. COPYRIGHT: (C)2008,JPO&INPIT
    • 待解决的问题:提供包含药物和浓度增强聚合物的药物组合物。 解决方案:组合物包含(a)溶解度改善形式的药物,其在给予使用环境时提供使用环境中的溶解药物浓度中的至少一种超过最低溶解度的平衡浓度 在使用环境中药物的形式以及在使用环境中超过药物溶解度最低的溶解速度的溶解速度,和(b)浓度增强聚合物以足够的量存在的浓度增强聚合物 使得该组合物在引入使用环境后提供使用环境中药物的最大浓度,其由对照组合物提供的药物的最大浓度为至少1.25倍,所述对照组合物的控制组合物为 药物在溶解性改善形式中单独使用,其中溶解度改善的药物形式选自纳米颗粒形式的药物,吸收 床上药物,纳米悬液中的药物,药物的过冷熔融物,环糊精/药物形式,明胶形式,软胶囊形式,自乳化形式和三相药物形式。 版权所有(C)2008,JPO&INPIT
    • 10. 发明专利
    • Drug
    • 药物
    • JP2007332141A
    • 2007-12-27
    • JP2007154664
    • 2007-06-12
    • Pfizer Prod Incファイザー・プロダクツ・インク
    • MAYER HOWARD BERNARD
    • A61K45/00A61K31/439A61P31/06A61P31/10A61P31/18A61P33/02A61P37/04A61P43/00
    • A61K31/439
    • PROBLEM TO BE SOLVED: To enhance the immune reconstitution of an HIV-infected patient, and hence treat HIV-associated oppotunistic symptoms caused by the immunocompromised state of the HIV patient. SOLUTION: This use of a CCR5 antagonist in the HIV-infected patient is to enhance the immune reconstitution of the patient for treating the HIV-associated oppotunistic symptoms caused by the immunocompromised state of the HIV patient. Since the patient having a CXCR4-using viral population obtains an advantage by the increase of the number of CD4 and/or CD8 cells, it becomes possible to treat such the patient by using the CCR5 antagonist. COPYRIGHT: (C)2008,JPO&INPIT
    • 要解决的问题:增强艾滋病毒感染患者的免疫重建,从而治疗由艾滋病毒患者的免疫受损状态引起的与艾滋病毒相关的对立症状。 解决方案:HIV感染患者中CCR5拮抗剂的使用是增强患者的免疫重建,用于治疗由HIV患者的免疫受损状态引起的与HIV相关的反应性症状。 由于患有CXCR4的病毒群体的患者通过CD4和/或CD8细胞的数量的增加获得了优势,所以可以通过使用CCR5拮抗剂来治疗这样的患者。 版权所有(C)2008,JPO&INPIT